Novel structures comprising phytosterol and/or phytostanol and ascorbic acid and use thereof in treating or preventing cardiovascular disease, its underlying conditions and other disorders

Abstract

Novel phytosterol and/or phytostanol derivatives, including salts thereof, are represented by the general formulae: wherein R is a phytosterol or phytostanol moiety, R2 is derived from ascorbic acid and R3 is hydrogen or any metal, alkali earth metal, or alkali metal. These derivatives are effective in treating and preventing cardiovascular disease and its underlying conditions including atherosclerosis and hyperlipidemia.

We claim:  
     
         1 . A chemical structure comprising phytosterol or phytostanol and ascorbic acid having one of the following formulae:  
       
         
           
           
               
               
           
         
       
       wherein R is a phytosterol or phytostanol moiety selected from the group consisting of sitosterol, campesterol, stigmasterol, brassicasterol, desmosterol, chalinosterol, poriferasterol, clionasterol, sitostanol, campestanol, stigmastanol, brassicastanol, desmostanol, chalinostanol, poriferastanol, and clionastanol; R2 is ascorbic acid and R3 is hydrogen or any metal, alkali earth metal, or alkali metal; or a salt thereof.  
     
     
         2 . The structure of  claim 1  wherein the phytosterol and phytostanol are in either a natural or synthesized form.  
     
     
         3 . The structure of  claim 1  wherein the phytosterol and phytostanol are in any one of their isomeric forms.  
     
     
         4 . The structure of  claim 1  wherein the phytostanol is sitostanol.  
     
     
         5 . The structure of  claim 1  wherein R3 is selected from the group consisting of calcium, magnesium, manganese, copper, zinc, sodium, potassium and lithium.  
     
     
         6  A composition for treating and preventing cardiovascular disease and its underlying conditions including atherosclerosis and hyperlipidemia, which comprises one or more of the structures having the following formulae:  
       
         
           
           
               
               
           
         
       
       wherein R is a phytosterol or phytostanol moiety selected from the group consisting of sitosterol, campesterol, stigmasterol, brassicasterol, desmosterol, chalinosterol, poriferasterol, clionasterol, sitostanol, campestanol, stigmastanol, brassicastanol, desmostanol, chalinostanol, poriferastanol, and clionastanol; R2 is ascorbic acid and R3 is hydrogen or any metal, alkali earth metal, or alkali metal; or a salt of these structures; and a pharmaceutically acceptable carrier therefore.  
     
     
         7 . The composition of  claim 6  wherein the phytosterol and phytostanol are in either a natural or synthesized form.  
     
     
         8 . The composition of  claim 6  wherein the phytosterol and phytostanol are in any one of their isomeric forms.  
     
     
         9 . The composition of  claim 6  wherein the phytostanol is sitostanol.  
     
     
         10 . The composition of  claim 6  wherein R3 is selected from the group consisting of calcium, magnesium, manganese, copper, zinc, sodium, potassium and lithium.  
     
     
         11 . The composition of  claim 6  additionally comprising at least one agent which reduces cholesterol synthesis in humans.  
     
     
         12 . The composition of  claim 11  wherein the agent is a 3-hydroxy-3-methyl glutaryl coenzyme-A (HMG-CoA) reductase inhibitor.  
     
     
         13 . A comestible or beverage which comprises one or more of the structures having the following formulae:  
       
         
           
           
               
               
           
         
       
       wherein R is a phytosterol or phytostanol moiety selected from the group consisting of sitosterol, campesterol, stigmasterol, brassicasterol, desmosterol, chalinosterol, poriferasterol, clionasterol, sitostanol, campestanol, stigmastanol, brassicastanol, desmostanol, chalinostanol, poriferastanol, and clionastanol; R2 is derived from ascorbic acid and R3 is hydrogen or any metal, alkali earth metal, or alkali metal; and all salts of these structures.  
     
     
         14 . The comestible or beverage of  claim 13  wherein the phytosterol and phytostanol are in either a natural or synthesized form.  
     
     
         15 . The comestible or beverage of  claim 13  wherein the phytosterol and phytostanol are in any one of their isomeric forms.  
     
     
         16 . The comestible or beverage of  claim 13  wherein the phytostanol is sitostanol.  
     
     
         17 . The comestible or beverage of  claim 13  wherein R3 is selected from the group consisting of calcium, magnesium, manganese, copper, zinc, sodium, potassium and lithium.  
     
     
         18 . The structure of  claim 1  wherein the phytostanol is campestanol.  
     
     
         19 . The composition of  claim 6  wherein the phytostanol is campestanol.  
     
     
         20 . The comestible or beverage of  claim 1  wherein the phytostanol is campestanol.